Torres Joana, Silva Renata, Farias Gonçalo, Sousa Lobo José Manuel, Ferreira Domingos Carvalho, Silva Ana Catarina
UCIBIO, Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.
Associate Laboratory i4HB Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.
Pharmaceutics. 2024 Oct 4;16(10):1297. doi: 10.3390/pharmaceutics16101297.
Migraine has a high prevalence worldwide and is one of the main disabling neurological diseases in individuals under the age of 50. In general, treatment includes the use of oral analgesics or non-steroidal anti-inflammatory drugs (NSAIDs) for mild attacks, and, for moderate or severe attacks, triptans or 5-HT receptor agonists. However, the administration of antimigraine drugs in conventional oral pharmaceutical dosage forms is a challenge, since many molecules have difficulty crossing the blood-brain barrier (BBB) to reach the brain, which leads to bioavailability problems. Efforts have been made to find alternative delivery systems and/or routes for antimigraine drugs. In vivo studies have shown that it is possible to administer drugs directly into the brain via the intranasal (IN) or the nose-to-brain route, thus avoiding the need for the molecules to cross the BBB. In this field, the use of lipid nanoparticles, in particular solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), has shown promising results, since they have several advantages for drugs administered via the IN route, including increased absorption and reduced enzymatic degradation, improving bioavailability. Furthermore, SLN and NLC are capable of co-encapsulating drugs, promoting their simultaneous delivery to the site of therapeutic action, which can be a promising approach for the acute migraine treatment. This review highlights the potential of using SLN and NLC to improve the treatment of acute migraine via the nose-to-brain route. First sections describe the pathophysiology and the currently available pharmacological treatment for acute migraine, followed by an outline of the mechanisms underlying the nose-to-brain route. Afterwards, the main features of SLN and NLC and the most recent in vivo studies investigating the use of these nanoparticles for the treatment of acute migraine are presented.
偏头痛在全球范围内具有较高的患病率，是50岁以下人群中主要的致残性神经疾病之一。一般来说，轻度发作的治疗包括使用口服镇痛药或非甾体抗炎药（NSAIDs），而中度或重度发作则使用曲坦类药物或5-羟色胺（5-HT）受体激动剂。然而，以传统口服药物剂型给药抗偏头痛药物是一项挑战，因为许多分子难以穿过血脑屏障（BBB）到达大脑，这导致了生物利用度问题。人们一直在努力寻找抗偏头痛药物的替代给药系统和/或给药途径。体内研究表明，通过鼻内（IN）或鼻-脑途径将药物直接注入大脑是可行的，从而避免了分子穿过血脑屏障的需要。在这一领域，脂质纳米颗粒，特别是固体脂质纳米颗粒（SLN）和纳米结构脂质载体（NLC），已显示出有前景的结果，因为它们对于通过鼻内途径给药的药物具有若干优势，包括吸收增加和酶降解减少，从而提高生物利用度。此外，SLN和NLC能够共包封药物，促进它们同时递送至治疗作用部位，这可能是急性偏头痛治疗的一种有前景的方法。本综述强调了使用SLN和NLC通过鼻-脑途径改善急性偏头痛治疗的潜力。第一部分描述了急性偏头痛的病理生理学和目前可用的药物治疗，随后概述了鼻-脑途径的潜在机制。之后，介绍了SLN和NLC的主要特征以及研究这些纳米颗粒用于急性偏头痛治疗的最新体内研究。
